Aclidinium bromide

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Aclidinium Bromide 抑制人毒蕈碱 AChR M1、M2、M3、M4 和 M5，Ki 分别为 0.1 nM、0.14 nM、0.14 nM、0.21 nM 和 0.16 nM。

Aclidinium Bromide inhibits human muscarinic AChR M1, M2, M3, M4 and M5 with Ki of 0.1 nM, 0.14 nM, 0.14 nM, 0.21 nM and 0.16 nM, respectively.(In Vitro):Preclinically, aclidinium showed potent antagonism of human muscarinic receptors, with a long residence time at M3 receptors and a shorter residence time at M2 receptors, indicating the potential to provide sustained bronchodilation. Aclidinium is rapidly hydrolysed in human plasma, unlike other currently available antimuscarinics including tiotropium. Early clinical studies in healthy subjects have confirmed the low systemic bioavailability and favourable safety profile of single and multiple doses of aclidinium. In a subsequent Phase IIb study, which included 464 patients with moderate to severe COPD, aclidinium displayed long-lasting bronchodilatory activity and was well tolerated.

Preclinically, aclidinium showed potent antagonism of human muscarinic receptors, with a long residence time at M3 receptors and a shorter residence time at M2 receptors, indicating the potential to provide sustained bronchodilation. Aclidinium is rapidly hydrolysed in human plasma, unlike other currently available antimuscarinics including tiotropium. Early clinical studies in healthy subjects have confirmed the low systemic bioavailability and favourable safety profile of single and multiple doses of aclidinium. In a subsequent Phase IIb study, which included 464 patients with moderate to severe COPD, aclidinium displayed long-lasting bronchodilatory activity and was well tolerated.

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LAS 34273 | LAS-W 330

Endocrinology/Hormones

AChR

M1 mAChR| M2 mAChR| M3 mAChR| M4 mAChR| M5 mAChR

Inflammation/Immunology

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320345-99-1

564.55

C26H30NO4S2·Br

>98% (HPLC)

DMSO: 113 mg/mL (200.15 mM)

O=C(O[C@H]1C[N+]2(CCCOC3=CC=CC=C3)CCC1CC2)C(C4=CC=CS4)(O)C5=CC=CS5.[Br-]

[(8R)-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octan-8-yl] 2-hydroxy-2,2-dithiophen-2-ylacetate bromide

(-20℃)

With Ice Pack

≥ 2 years